WO2023014296A3 - Molecular glue and sall4 degrader - Google Patents

Molecular glue and sall4 degrader Download PDF

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Publication number
WO2023014296A3
WO2023014296A3 PCT/SG2022/050551 SG2022050551W WO2023014296A3 WO 2023014296 A3 WO2023014296 A3 WO 2023014296A3 SG 2022050551 W SG2022050551 W SG 2022050551W WO 2023014296 A3 WO2023014296 A3 WO 2023014296A3
Authority
WO
WIPO (PCT)
Prior art keywords
sall4
degrader
molecular glue
cancer
compounds
Prior art date
Application number
PCT/SG2022/050551
Other languages
French (fr)
Other versions
WO2023014296A2 (en
Inventor
Le Kim Anh VU
Bee Hui Liu
Daniel Geoffrey TENEN
Original Assignee
National University Of Singapore
Beth Israel Deaconess Medical Center, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by National University Of Singapore, Beth Israel Deaconess Medical Center, Inc. filed Critical National University Of Singapore
Priority to EP22853619.9A priority Critical patent/EP4380557A2/en
Publication of WO2023014296A2 publication Critical patent/WO2023014296A2/en
Publication of WO2023014296A3 publication Critical patent/WO2023014296A3/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/17—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
    • A61K31/175—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine having the group, >N—C(O)—N=N— or, e.g. carbonohydrazides, carbazones, semicarbazides, semicarbazones; Thioanalogues thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/423—Oxazoles condensed with carbocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Provided is the use of compounds of Formula I, as well as certain specific compounds, or a pharmaceutically acceptable salt, solvate or derivative thereof, in the preparation of a medicament to treat cancer, such as liver cancer (e.g. hepatocellular carcinoma) and lung cancer.
PCT/SG2022/050551 2021-08-02 2022-08-02 Molecular glue and sall4 degrader WO2023014296A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP22853619.9A EP4380557A2 (en) 2021-08-02 2022-08-02 Molecular glue and sall4 degrader

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202163228240P 2021-08-02 2021-08-02
US63/228,240 2021-08-02

Publications (2)

Publication Number Publication Date
WO2023014296A2 WO2023014296A2 (en) 2023-02-09
WO2023014296A3 true WO2023014296A3 (en) 2023-04-27

Family

ID=85156467

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/SG2022/050551 WO2023014296A2 (en) 2021-08-02 2022-08-02 Molecular glue and sall4 degrader

Country Status (2)

Country Link
EP (1) EP4380557A2 (en)
WO (1) WO2023014296A2 (en)

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20130156795A1 (en) * 2009-09-01 2013-06-20 Antonio Iavarone Methods for inhibition of cell proliferation, synergistic transcription modules and uses thereof
US20150210717A1 (en) * 2012-09-13 2015-07-30 Baden-Württemberg Stiftung Gmbh Specific inhibitors of protein p21 as therapeutic agents
CN106496108A (en) * 2016-11-01 2017-03-15 上海应用技术大学 There is amides compound and its application of anti-tumor activity
WO2019070943A1 (en) * 2017-10-04 2019-04-11 Dana-Farber Cancer Institute, Inc. Small molecule inhibition of transcription factor sall4 and uses thereof
WO2020123675A1 (en) * 2018-12-11 2020-06-18 Duke University Compositions and methods for the treatment of cancer
WO2020242376A1 (en) * 2019-05-28 2020-12-03 Agency For Science, Technology And Research Method of treating a sall4-expressing cancer

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20130156795A1 (en) * 2009-09-01 2013-06-20 Antonio Iavarone Methods for inhibition of cell proliferation, synergistic transcription modules and uses thereof
US20150210717A1 (en) * 2012-09-13 2015-07-30 Baden-Württemberg Stiftung Gmbh Specific inhibitors of protein p21 as therapeutic agents
CN106496108A (en) * 2016-11-01 2017-03-15 上海应用技术大学 There is amides compound and its application of anti-tumor activity
WO2019070943A1 (en) * 2017-10-04 2019-04-11 Dana-Farber Cancer Institute, Inc. Small molecule inhibition of transcription factor sall4 and uses thereof
WO2020123675A1 (en) * 2018-12-11 2020-06-18 Duke University Compositions and methods for the treatment of cancer
WO2020242376A1 (en) * 2019-05-28 2020-12-03 Agency For Science, Technology And Research Method of treating a sall4-expressing cancer

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
HU, W.P. ET AL.: "Synthesis and biological evaluation of thiobenzanilides as anticancer agents", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 16, no. 9, 6 March 2008 (2008-03-06), pages 5295 - 5302, XP022647320, [retrieved on 20230328], DOI: 10.1016/J.BMC. 2008.03.00 3 *
KENLAN, D.E. ET AL.: "Fluorinated N,N'-Diarylureas As Novel Therapeutic Agents Against Cancer Stem Cells", MOLECULAR CANCER THERAPEUTICS, vol. 16, no. 5, 2 May 2017 (2017-05-02), pages 831 - 837, XP055876037, [retrieved on 20230328], DOI: 10.1158/1535-7163.MCT-15-0634 *
XU TIAN, ZHANG JIFA, YANG CHENGCAN, PLUTA RYSZARD, WANG GUAN, YE TINGHONG, OUYANG LIANG: "Identification and optimization of 3-bromo-N’-(4-hydroxybenzylidene)-4-methylbenzohydrazide derivatives as mTOR inhibitors that induce autophagic cell death and apoptosis in triple-negative breast cancer", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, ELSEVIER, AMSTERDAM, NL, vol. 219, 1 July 2021 (2021-07-01), AMSTERDAM, NL , pages 113424, XP093064991, ISSN: 0223-5234, DOI: 10.1016/j.ejmech.2021.113424 *
ZHANG YUAN, MENG XIN, TANG HAIKANG, CHENG MINGHUI, YANG FUJUN, XU WENQING: "Design, synthesis, and biological evaluation of novel substituted thiourea derivatives as potential anticancer agents for NSCLC by blocking K-Ras protein-effectors interactions", JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, INFORMA HEALTHCARE, GB, vol. 35, no. 1, 1 January 2020 (2020-01-01), GB , pages 344 - 353, XP093064990, ISSN: 1475-6366, DOI: 10.1080/14756366.2019.1702653 *
ZHU, Z.W. ET AL.: "Synthesis and antiproliferative activities against Hep-G2 of salicylanide derivatives: potent inhibitors of the epidermal growth factor receptor (EGFR) tyrosine kinase", JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 26, no. 1, 28 June 2010 (2010-06-28), pages 37 - 45, XP055663729, [retrieved on 20230328], DOI: 10.3109/14756361003671060 *

Also Published As

Publication number Publication date
WO2023014296A2 (en) 2023-02-09
EP4380557A2 (en) 2024-06-12

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